EP 3383421 A4 20190724 - STAPLED HELICAL PEPTIDES AND METHODS OF SYNTHESIS
Title (en)
STAPLED HELICAL PEPTIDES AND METHODS OF SYNTHESIS
Title (de)
GEKLAMMERTE SPIRALFÖRMIGE PEPTIDE UND VERFAHREN ZUR SYNTHESE
Title (fr)
PEPTIDES HÉLICOÏDAUX AGRAFÉS ET LEURS PROCÉDÉS DE SYNTHÈSE
Publication
Application
Priority
- US 201562261395 P 20151201
- CN 2016108210 W 20161201
Abstract (en)
[origin: US2017152286A1] The present disclosure relates to the design and generation of stapled helical peptides that perturb protein-protein interactions (PPIs). The methods disclosed herein for preparing stapled peptides involve providing a peptide having a first amino acid that is functionalized with a salicylaldehyde ester side group and a second amino acid functionalized with a 1,2-hydroxyl amine side group; reacting the first and second amino acids to generate an N,O-benzylidene acetal moiety; and performing acidolysis of the resultant N,O-benzylidene acetal moiety to generate the stapled peptide. In many forms, the stapled helical peptides described herein are not hydrophobic.
IPC 8 full level
C07K 1/107 (2006.01); A61K 38/16 (2006.01); C07K 7/56 (2006.01); C07K 14/00 (2006.01)
CPC (source: EP US)
C07K 1/1075 (2013.01 - EP US); C07K 1/122 (2013.01 - US); C07K 7/56 (2013.01 - EP US); C07K 7/64 (2013.01 - US); C07K 14/001 (2013.01 - US); A61K 38/00 (2013.01 - EP US)
Citation (search report)
- [XAI] WO 9411393 A1 19940526 - SALK INST FOR BIOLOGICAL STUDI [US]
- [A] CLARENCE T. T. WONG ET AL: "Synthesis of Constrained Head-to-Tail Cyclic Tetrapeptides by an Imine-Induced Ring-Closing/Contraction Strategy", ANGEWANDTE CHEMIE, INTERNATIONAL EDITION, vol. 52, no. 39, 23 September 2013 (2013-09-23), DE, pages 10212 - 10215, XP055597130, ISSN: 1433-7851, DOI: 10.1002/anie.201304773
- See references of WO 2017092691A1
Designated contracting state (EPC)
AL AT BE BG CH CY CZ DE DK EE ES FI FR GB GR HR HU IE IS IT LI LT LU LV MC MK MT NL NO PL PT RO RS SE SI SK SM TR
DOCDB simple family (publication)
US 10011631 B2 20180703; US 2017152286 A1 20170601; CN 109069581 A 20181221; CN 109069581 B 20210713; EP 3383421 A1 20181010; EP 3383421 A4 20190724; EP 3383421 B1 20210519; WO 2017092691 A1 20170608
DOCDB simple family (application)
US 201615363626 A 20161129; CN 2016108210 W 20161201; CN 201680080440 A 20161201; EP 16870001 A 20161201